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抑制剂选择性比较

Rho产品

所有产品(17) Rho抑制剂(16) Rho激活剂(1)

目录号	产品描述	文献引用	实验数据
S1573	Fasudil (HA-1077) HCl Fasudil (HA-1077, AT-877)是一种有效的、具有选择性的Rho抑制剂（ROCK2, Ki=0.33 μM），同时对PKA、PKG、PKC和MLCK也具有抑制活性，Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。	Proc Natl Acad Sci U S A, 2021, 118(2)e2016034118 Int J Neurosci, 2021, 1-7 Nat Cell Biol, 2020, 25	The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.
S1314	Zoledronic Acid Zoledronic acid (ZA, Zoledronate, CGP-4244, GP42446A, ZOL 446, Zometa, Zomera, Aclasta, Reclast), 破骨细胞抑制剂，通过抑制甲羟戊酸途径诱导破骨细胞凋亡，并防止小GTP结合蛋白，如Ras 和 Rho的异戊二烯化。Zoledronic acid (ZA) 还可诱导自噬。	Aging Cell, 2020, 29 Cancers (Basel), 2020, 31;12(1) pii: E104 Mol Cancer Ther, 2020, 19(1):39-51	Isolation of cd T cells. PBMCs were cultured in the presence of 400 nM ZA and 200 IU/ml IL-2 over 10 days. cd T cells were isolated by negative MACS isolation. Flow cytometric analysis revealed co-expression of CD3 and TCRcd on over 99% of cells of the flow through fraction (A). The T cells expressed the TCRVd2 chain (B) and the CD56 protein (C).
S8031	NSC 23766 NSC 23766是一种Rac GTPase抑制剂，通过鸟嘌呤核苷酸因子(GEFs)靶向作用于Rac 活化，无细胞试验中IC50为~50 μM；但是不会抑制密切相关的靶点，Cdc42或RhoA。	Dig Dis Sci, 2021, 10.1007/s10620-020-06812-3 Nat Commun, 2020, 19;11(1):1456 Autophagy, 2020, 28;1-16	MES cells were treated with Rac inhibitor (50 μM EHT1864 or NSC23766) and assayed for self-renewal by serial passage mammosphere formation. P1, passage 1; P2, passage 2. Data are means ± SEM of three biological replicates. *P ≤ 0.05 by two-tailed t test.
S7319	EHop-016 EHop-016 是一种特异性Rac GTPase抑制剂，在MDA-MB-435 和 MDA-MB-231细胞中作用于Rac1，IC50为1.1 μM，同等有效抑制Rac3。	PLoS Genet, 2020, 16(3):e1008694 Stem Cell Res Ther, 2020, 11(1):525 Sci Rep, 2020, 10(1):21018	(f) Liver samples from both groups treated with olive oil, CCl4, CCl4+NSC23766 or +EHop-016 for 4 weeks were collected for Rac1 activity assay and western blot analysis.
S1721	Azathioprine Azathioprine 是一种抑制免疫系统的药物，抑制了嘌呤的合成以及GTP结合蛋白Rac1的激活，用于器官移植和自身免疫性疾病。	Sci Rep, 2019, 9(1):4360 Blood, 2016, 1;128(9):1234-45
S0890^New	MLS000532223 MLS000532223 是一种 Rho family GTPases 的高亲和力的选择性抑制剂，EC50值为16 μM至120 μM。
S8988^New	Rhosin hydrochloride Rhosin (G04) hydrochloride (HCl) 是RhoA亚家族 Rho GTPases 的强效特异性抑制剂，Kd值约为0.4 uM。Rhosin hydrochloride 可诱导细胞凋亡。
S7293	ZCL278 ZCL278是一个选择性的Cdc42 GTP酶抑制剂，Kd为11.4 μM。	EBioMedicine, 2019, 50:122-134 J Cell Physiol, 2018, 10.1002/jcp.27510 J Bone Miner Res, 2018, 33(5):945-958	Rho GTPases were involved in NaAsO2 induced apoptosis in rat CGNs. A. Representative fluorescence images of cells exposed to 0 and 10 μM NaAsO2 for 24 h with or without ZCL278 (an inhibitor of Cdc42), or a Rac1 inhibitor NSC23766. Both ZCL278 and NSC23766 reduced the apoptotic cells. B. The graph indicates TUNEL-positive rat CGNs exposed to NaAsO2 (10 μM) with ZCL278 or NSC23766 groups decreased significantly compared with those of NaAsO2 treatment group. Data are expressed as mean ± SD from at least 5 visual fields. C. Rat CGNs in 96-well plates were treated by 0 and 10 μM NaAsO2 for 24h with or without ZCL278 (an inhibitor of Cdc42) pretreatment for 1 h, or a Rac1 inhibitor NSC23766 pretreatment for 12 h, and assessed by a CCK-8. ZCL278 and NSC23766 increased rat CGNs viability exposed to NaAsO2. All statistical results are expressed as means±SD from at least three independent experiments. ***P<0.001 vs control, # P<0.05, ##P<0.01, ###P<0.001 VS NaAsO2 treatment group.
S8749	MBQ-167 MBQ-167是一种有效的Rac和Cdc42双重抑制剂，在转移性乳腺癌细胞中，IC50分别为103 nM和78 nM。	Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19 PLoS One, 2020, 15(6):e0235116
S7719	CCG-1423 CCG-1423是一种特定的 RhoA 通路抑制剂，能够抑制SRF介导的转录。	Nat Commun, 2020, 11(1):3282 Front Cell Dev Biol, 2020, 8:839 J Cell Sci, 2020, jcs.238840	Cells were treated with CCG-1423 for 48 h. CCG-1423 blocked the nuclear translocation of MRTF-A.
S8469	CCG-203971 CCG-203971是一种新型的Rho/MRTF/SRF通路抑制剂，对SRE.L.的IC50值为0.64 μM。它可以抑制Rho介导的基因转录。	J Cell Physiol, 2020, 235(5):4790-4803 Small GTPases, 2020, 10.1080/21541248
S6673	CCG-222740 CCG-222740是一种Rho/MRTF通路抑制剂。CCG-222740通过降低α平滑肌肌动蛋白(alpha smooth muscle actin, α-SMA)的表达水平来降低星状细胞在体外和体内的活化。
S7482	EHT 1864 2HCl EHT 1864 2HCl是一种强效的Rac family GTPase抑制剂，其对Rac1, Rac1b, Rac2 和 Rac3的K_d分别为40 nM, 50 nM, 60 nM 和 250 nM 。	Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19 Viruses, 2020, 12(10)E1128	E) Representative images of 3-dimensional visualization of vessel networks, H&E staining, and Masson staining. Dotted straight line indicates the femur—implant junction (F, femur; I, implant). Black box, implant region; blue arrows, osteocytes; yellow arrows, osteoblast cells; black triangle, newly formed bone or implant debris, black arrows, chondrocyte-like cells; red triangle, blood sinus. Scale bars, 200 μm.
S7686	ML141 ML141 (CID-2950007) 是 Rho 家族GTPase cdc42的一种有效的，选择性可逆非竞争性抑制剂，IC50为200 nM。对cdc42比对其他Rho家族中的GTPases(如Rac1, Rab2, Rab7)更有选择性。 ML141 与 p38 激活增加有关，并可能诱导p38依赖性凋亡/衰老。ML141还可保护神经母细胞瘤细胞免受二甲双胍(metformin)诱导的凋亡。	Micromachines (Basel), 2021, 12(2)112 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19	(A) The survival rate detected at 72 h after the injection of different concentrations of ML141; shrimp injected with DMSO were used as controls. (B) The expression of WSSV IE1 at the mRNA level at 24 h post ML141 injection. Shrimp injected with the same amount of DMSO in each group were used as controls.
S5244	Zoledronic acid monohydrate Zoledronic acid (Zoledronate, CGP-4244) monohydrate 是 Zoledronic acid (唑来膦酸) 的一水合物，是有效的破骨细胞抑制剂，可通过抑制甲戊二羟酸途径的酶、阻止小GTP结合蛋白如Ras和Rho的异戊二烯化来诱导破骨细胞凋亡。	Cancers (Basel), 2020, 31;12(1) pii: E104 J Cell Mol Med, 2020, 25 Oncol Rep, 2020, 45(2):459-468
S6752	Y16 Y16是G蛋白偶联Rho GEFs抑制剂。它能阻止LARG和Rho的结合，Kd值为80 nM。
S0765^New	MAZ51 MAZ51 是一种选择性的 vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase 的有效抑制剂。MAZ51 通过 Akt/GSK3β 的磷酸化和 RhoA 的激活来诱导神经胶质瘤细胞的细胞圆缩和G2/M细胞周期停滞。 MAZ51 可抑制多种非VEGFR-3表达肿瘤细胞的增殖并诱导其凋亡。

目录号	产品描述	文献引用	实验数据
S1573	Fasudil (HA-1077) HCl Fasudil (HA-1077, AT-877)是一种有效的、具有选择性的Rho抑制剂（ROCK2, Ki=0.33 μM），同时对PKA、PKG、PKC和MLCK也具有抑制活性，Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。	Proc Natl Acad Sci U S A,2021, 118(2)e2016034118 Int J Neurosci,2021, 1-7 Nat Cell Biol,2020, 25	The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.
S1314	Zoledronic Acid Zoledronic acid (ZA, Zoledronate, CGP-4244, GP42446A, ZOL 446, Zometa, Zomera, Aclasta, Reclast), 破骨细胞抑制剂，通过抑制甲羟戊酸途径诱导破骨细胞凋亡，并防止小GTP结合蛋白，如Ras 和 Rho的异戊二烯化。Zoledronic acid (ZA) 还可诱导自噬。	Aging Cell,2020, 29 Cancers (Basel),2020, 31;12(1) pii: E104 Mol Cancer Ther,2020, 19(1):39-51	Isolation of cd T cells. PBMCs were cultured in the presence of 400 nM ZA and 200 IU/ml IL-2 over 10 days. cd T cells were isolated by negative MACS isolation. Flow cytometric analysis revealed co-expression of CD3 and TCRcd on over 99% of cells of the flow through fraction (A). The T cells expressed the TCRVd2 chain (B) and the CD56 protein (C).
S8031	NSC 23766 NSC 23766是一种Rac GTPase抑制剂，通过鸟嘌呤核苷酸因子(GEFs)靶向作用于Rac 活化，无细胞试验中IC50为~50 μM；但是不会抑制密切相关的靶点，Cdc42或RhoA。	Dig Dis Sci,2021, 10.1007/s10620-020-06812-3 Nat Commun,2020, 19;11(1):1456 Autophagy,2020, 28;1-16	MES cells were treated with Rac inhibitor (50 μM EHT1864 or NSC23766) and assayed for self-renewal by serial passage mammosphere formation. P1, passage 1; P2, passage 2. Data are means ± SEM of three biological replicates. *P ≤ 0.05 by two-tailed t test.
S7319	EHop-016 EHop-016 是一种特异性Rac GTPase抑制剂，在MDA-MB-435 和 MDA-MB-231细胞中作用于Rac1，IC50为1.1 μM，同等有效抑制Rac3。	PLoS Genet,2020, 16(3):e1008694 Stem Cell Res Ther,2020, 11(1):525 Sci Rep,2020, 10(1):21018	(f) Liver samples from both groups treated with olive oil, CCl4, CCl4+NSC23766 or +EHop-016 for 4 weeks were collected for Rac1 activity assay and western blot analysis.
S1721	Azathioprine Azathioprine 是一种抑制免疫系统的药物，抑制了嘌呤的合成以及GTP结合蛋白Rac1的激活，用于器官移植和自身免疫性疾病。	Sci Rep,2019, 9(1):4360 Blood,2016, 1;128(9):1234-45
S0890^New	MLS000532223 MLS000532223 是一种 Rho family GTPases 的高亲和力的选择性抑制剂，EC50值为16 μM至120 μM。
S8988^New	Rhosin hydrochloride Rhosin (G04) hydrochloride (HCl) 是RhoA亚家族 Rho GTPases 的强效特异性抑制剂，Kd值约为0.4 uM。Rhosin hydrochloride 可诱导细胞凋亡。
S7293	ZCL278 ZCL278是一个选择性的Cdc42 GTP酶抑制剂，Kd为11.4 μM。	EBioMedicine,2019, 50:122-134 J Cell Physiol,2018, 10.1002/jcp.27510 J Bone Miner Res,2018, 33(5):945-958	Rho GTPases were involved in NaAsO2 induced apoptosis in rat CGNs. A. Representative fluorescence images of cells exposed to 0 and 10 μM NaAsO2 for 24 h with or without ZCL278 (an inhibitor of Cdc42), or a Rac1 inhibitor NSC23766. Both ZCL278 and NSC23766 reduced the apoptotic cells. B. The graph indicates TUNEL-positive rat CGNs exposed to NaAsO2 (10 μM) with ZCL278 or NSC23766 groups decreased significantly compared with those of NaAsO2 treatment group. Data are expressed as mean ± SD from at least 5 visual fields. C. Rat CGNs in 96-well plates were treated by 0 and 10 μM NaAsO2 for 24h with or without ZCL278 (an inhibitor of Cdc42) pretreatment for 1 h, or a Rac1 inhibitor NSC23766 pretreatment for 12 h, and assessed by a CCK-8. ZCL278 and NSC23766 increased rat CGNs viability exposed to NaAsO2. All statistical results are expressed as means±SD from at least three independent experiments. ***P<0.001 vs control, # P<0.05, ##P<0.01, ###P<0.001 VS NaAsO2 treatment group.
S8749	MBQ-167 MBQ-167是一种有效的Rac和Cdc42双重抑制剂，在转移性乳腺癌细胞中，IC50分别为103 nM和78 nM。	Cell,2020, 182(3):685-712.e19 Cell,2020, 182(3):685-712.e19 PLoS One,2020, 15(6):e0235116
S7719	CCG-1423 CCG-1423是一种特定的 RhoA 通路抑制剂，能够抑制SRF介导的转录。	Nat Commun,2020, 11(1):3282 Front Cell Dev Biol,2020, 8:839 J Cell Sci,2020, jcs.238840	Cells were treated with CCG-1423 for 48 h. CCG-1423 blocked the nuclear translocation of MRTF-A.
S8469	CCG-203971 CCG-203971是一种新型的Rho/MRTF/SRF通路抑制剂，对SRE.L.的IC50值为0.64 μM。它可以抑制Rho介导的基因转录。	J Cell Physiol,2020, 235(5):4790-4803 Small GTPases,2020, 10.1080/21541248
S6673	CCG-222740 CCG-222740是一种Rho/MRTF通路抑制剂。CCG-222740通过降低α平滑肌肌动蛋白(alpha smooth muscle actin, α-SMA)的表达水平来降低星状细胞在体外和体内的活化。
S7482	EHT 1864 2HCl EHT 1864 2HCl是一种强效的Rac family GTPase抑制剂，其对Rac1, Rac1b, Rac2 和 Rac3的K_d分别为40 nM, 50 nM, 60 nM 和 250 nM 。	Cell,2020, 182(3):685-712.e19 Cell,2020, 182(3):685-712.e19 Viruses,2020, 12(10)E1128	E) Representative images of 3-dimensional visualization of vessel networks, H&E staining, and Masson staining. Dotted straight line indicates the femur—implant junction (F, femur; I, implant). Black box, implant region; blue arrows, osteocytes; yellow arrows, osteoblast cells; black triangle, newly formed bone or implant debris, black arrows, chondrocyte-like cells; red triangle, blood sinus. Scale bars, 200 μm.
S7686	ML141 ML141 (CID-2950007) 是 Rho 家族GTPase cdc42的一种有效的，选择性可逆非竞争性抑制剂，IC50为200 nM。对cdc42比对其他Rho家族中的GTPases(如Rac1, Rab2, Rab7)更有选择性。 ML141 与 p38 激活增加有关，并可能诱导p38依赖性凋亡/衰老。ML141还可保护神经母细胞瘤细胞免受二甲双胍(metformin)诱导的凋亡。	Micromachines (Basel),2021, 12(2)112 Cell,2020, 182(3):685-712.e19 Cell,2020, 182(3):685-712.e19	(A) The survival rate detected at 72 h after the injection of different concentrations of ML141; shrimp injected with DMSO were used as controls. (B) The expression of WSSV IE1 at the mRNA level at 24 h post ML141 injection. Shrimp injected with the same amount of DMSO in each group were used as controls.
S5244	Zoledronic acid monohydrate Zoledronic acid (Zoledronate, CGP-4244) monohydrate 是 Zoledronic acid (唑来膦酸) 的一水合物，是有效的破骨细胞抑制剂，可通过抑制甲戊二羟酸途径的酶、阻止小GTP结合蛋白如Ras和Rho的异戊二烯化来诱导破骨细胞凋亡。	Cancers (Basel),2020, 31;12(1) pii: E104 J Cell Mol Med,2020, 25 Oncol Rep,2020, 45(2):459-468
S6752	Y16 Y16是G蛋白偶联Rho GEFs抑制剂。它能阻止LARG和Rho的结合，Kd值为80 nM。

目录号	产品描述	文献引用	实验数据
S0765^New	MAZ51 MAZ51 是一种选择性的 vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase 的有效抑制剂。MAZ51 通过 Akt/GSK3β 的磷酸化和 RhoA 的激活来诱导神经胶质瘤细胞的细胞圆缩和G2/M细胞周期停滞。 MAZ51 可抑制多种非VEGFR-3表达肿瘤细胞的增殖并诱导其凋亡。

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S0765^New

MAZ51

MAZ51 是一种选择性的 vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase 的有效抑制剂。MAZ51 通过 Akt/GSK3β 的磷酸化和 RhoA 的激活来诱导神经胶质瘤细胞的细胞圆缩和G2/M细胞周期停滞。 MAZ51 可抑制多种非VEGFR-3表达肿瘤细胞的增殖并诱导其凋亡。

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抑制剂选择性比较

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